Trimedoxime
Trimedoxime (TMB-4) is a blood-brain barrier-permeable cholinesterase reactivator. Trimedoxime reactivates cholinesterase inhibited by paraoxon, sarin, tabun and other agents, restricts the breakdown of acetylcholine and alleviates excessive cholinergic stimulation. Trimedoxime reduces mortality and prolongs survival time. Trimedoxime exhibits reactivation efficacy against AChE in rat tissues. Trimedoxime can be used in research related to organophosphate (paraoxon) poisoning and tabun poisoning.
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- No. CAS: 56-97-3
- Fòrmula: C15H18Br2N4O2
- Peso molecular:446.14
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Trimedoxime (7.5 mg/kg; i.m.; single dose) significantly reactivates acetylcholinesterase (AChE) inhibited by tabun in rat blood and diaphragm, with reactivation rates of 17.5% and 34.7%, respectively, but exerts extremely weak reactivation on this enzyme in rat brain (only 2.8%), and reduces the acute lethal effect of tabun in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 200-250 g, organophosphate poisoning model via intraperitoneal paraoxon exposure)[1]
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Dosage:25 µM/rat
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Administration:i.p.; single dose
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Result:Reduced 48-hour mortality to 38% in rats exposed to 1 µmol/rat paraoxon.
Reduced 48-hour mortality to 76% in rats exposed to 10 µmol/rat paraoxon.
Reduced 48-hour mortality to 83% in rats exposed to 15 µmol/rat paraoxon.
Lowered the relative risk of death to 0.36 (95% confidence interval, 0.26 to 0.50) compared to paraoxon-only controls.
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Animal Model:Wistar (male, 180-200 g, tabun poisoning model)[3]
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Dosage:7.5 mg/kg
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Administration:i.m.; single prophylactic dose
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Result:Produced 17.5% reactivation of tabun-inhibited AChE in blood.
Produced 34.7% reactivation of tabun-inhibited AChE in diaphragm.
Produced 2.8% reactivation of tabun-inhibited AChE in brain.
Showed significant differences from atropine-only control and HI-6 treatment group.
Increased the LD50 of tabun in mice to 504.8 μg/kg.
Resulted in a protective ratio of 1.71.
Showed significant difference from untreated group and HI-6 treatment group.
Chemical Information
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No. CAS 56-97-3
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Peso molecular 446.14
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Fòrmula C15H18Br2N4O2
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SMILES
O/N=C/C1=CC=[N+](CCC[N+]2=CC=C(C=C2)/C=N/O)C=C1.[Br-].[Br-]
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Synonyms
TMB-4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Trimedoxime Related Classifications
HY-165600A Related Classifications
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